- Inhibitor of heat shock factor 1, and preparation method and application of inhibitor
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The invention provides an inhibitor of a heat shock factor 1 (HSF1) and an application of the inhibitor, particularly a compound as shown in a formula I or pharmaceutically-acceptable salt of the compound. The compound has excellent HSF1 restraining activity and tumor resisting effects. The invention further provides a medical composition containing the compound and an application of the medical composition in the respect of restraining HSF1.
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Paragraph 0191; 0202-0204
(2019/12/08)
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- S - Cis Diene Conformation: A New Bathochromic Shift Strategy for Near-Infrared Fluorescence Switchable Dye and the Imaging Applications
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In this paper, we present a novel charge-free fluorescence-switchable near-infrared (IR) dye based on merocyanine for target specific imaging. In contrast to the typical bathochromic shift approach by extending π-conjugation, the bathochromic shift of our merocyanine dye to the near-IR region is due to an unusual S-cis diene conformer. This is the first example where a fluorescent dye adopts the stable S-cis conformation. In addition to the novel bathochromic shift mechanism, the dye exhibits fluorescence-switchable properties in response to polarity and viscosity. By incorporating a protein-specific ligand to the dye, the probes (for SNAP-tag and hCAII proteins) exhibited dramatic fluorescence increase (up to 300-fold) upon binding with its target protein. The large fluorescence enhancement, near-IR absorption/emission, and charge-free scaffold enabled no-wash and site-specific imaging of target proteins in living cells and in vivo with minimum background fluorescence. We believe that our unconventional approach for a near-IR dye with the S-cis diene conformation can lead to new strategies for the design of near-IR dyes.
- Chen, Hsiang-Jung,Chew, Chee Ying,Chang, En-Hao,Tu, Yu-Wei,Wei, Li-Yu,Wu, Bo-Han,Chen, Chien-Hung,Yang, Ya-Ting,Huang, Su-Chin,Chen, Jen-Kun,Chen, I-Chia,Tan, Kui-Thong
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supporting information
p. 5224 - 5234
(2018/04/23)
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- Design, synthesis and biological evaluation of some novel N-arylpyrazole derivatives bearing the sulfonamide moiety as cytotoxic agents
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A series of novel N-arylpyrazole derivatives (4a–4l) bearing the sulfonamide moiety were synthesized by the condensation reaction of 1,3-dicarbonyl compounds with 4-hydrazinylbenzenesulfonamide. The structures of the obtained compounds were established on
- Duan, Xiaobo,Wang, Yingxing,Feng, Weipei,Yang, Yaxing,Li, Hongyan,Li, Shenghui,Yang, Xiaobing,Zhang, Jinchao,Wang, Shuxiang,Zhou, Guoqiang,Zhou, Chuanqi
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p. 271 - 281
(2017/01/14)
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- Synthesis, anticancer activity and DNA-binding properties of novel 4-pyrazolyl-1,8-naphthalimide derivatives
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A novel series of 4-pyrazolyl-1,8-naphthalimide derivatives have been designed and facilely synthesized. For anticancer activity in vitro, most of the compounds were found to be more toxic against human mammary cancer cells (MCF-7) than human cervical car
- Li, Shenghui,Xu, Shengjie,Tang, Yonghe,Ding, Shan,Zhang, Jinchao,Wang, Shuxiang,Zhou, Guoqiang,Zhou, Chuanqi,Li, Xiaoliu
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supporting information
p. 586 - 590
(2014/01/23)
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- Synthesis and biological evaluation of some novel N-arylpyrazole derivatives as cytotoxic agents
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A series of novel N-arylpyrazole derivatives, 5a-5i, were achieved from substituted phenylacetic acid via Vilsmeier-Haack reaction, hydrolysis, condensation, and aromatic substitution reaction. Their chemical structures were confirmed by 1H NMR
- Li, Shenghui,Xu, Shengjie,Ding, Shan,Zhang, Jinchao,Wang, Shuxiang,Li, Xiaoliu
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p. 1459 - 1468
(2014/05/06)
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